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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
141 NEW CALPAIN-INHIBITOR KP-1241 AND ITS PRODUCTION JP1900193 1993-02-05 JPH0641067A 1994-02-15 OMURA SATOSHI; TANAKA HARUO; SHIOMI KAZURO; RIYUU JIN RON
A compound of formula: or a pharmaceutically or veterinarilly acceptable salt thereof, is useful as a calpain inhibitor.
142 THIOCARBAMOYLACETONITRILE DERIVATIVE JP22441291 1991-09-04 JPH0558997A 1993-03-09 NIIFUKU TETSUO; BESSHO HIDEKI; KIYONO ASAMI; HAYASHI JUNKO
PURPOSE:To obtain the subject new acetonitrile derivative, having a specific aryl group substituted at the alpha-position of acetonitrile and excellent hypotensive and vasodilator actions and useful as an oral or a parenteral antihypertensive agent for treating hypertension, etc. CONSTITUTION:A compound expressed by formula I [R<1> is H, 1-6C alkyl, etc.; Ar is (substituted)benzene ring; X is the formula (CH2)m ((m)is 0 or 1-3) or CO; Y is 5- or 6-membered ring (substituted) heterocyclic ring, condensed heterocyclic ring, etc.]{e.g. 2-[4-(1,2,4-triazol-5-yl)-phenyl]-propionitrile} is dissolved in tetrahydrofuran. Methyl isothiocyanate is then added to the solution and the above-mentioned compound is reacted with the methyl isocyanate in the presence of potassium tert. butoxide for 2 hr while being cooled with ice. Aqueous hydrochloric acid is subsequently added to neutralize the reaction mixture, which is then extracted with ethyl acetate. The extracted compound is purified by silica gel column chromatography to afford the objective thiocarbamoylacetonitrile derivative expressed by 2 formula II (R<2> is 1-10C alkyl).
143 BUTENOIC ACID DERIVATIVE JP13989689 1989-06-01 JPH0395157A 1991-04-19 MINAMI NORIO; OZAKI FUMIHIRO; ISHIBASHI KEIJI; KABASAWA YASUHIRO; IKEMORI MEGUMI; OGAWA TOSHIAKI; KAWAMURA TAKANORI
NEW MATERIAL:A compound expressed by formula I [R<1> is hetroaryl; R<2> and R<3> are H, lower alkyl, cycloalkyl or allyl; A is 1-6C alkylene; X is O, S, vinylene, etc.; J is formula II (R<4> to R<6> are H, halogen, lower alkyl, hydroxy, nitro, etc.) or pyridyl; (n) is 1-6] or salt thereof. EXAMPLE:(E)-N-[3-((N'-(2-(3,5-Dimethoxyphenyl)ethyl)-N'-methyl)amino) propyl]-4-(4-(1H-imidazol-1-yl)phenyl)-3-butenamide. USE:A treating, preventive and improving agent for ischemic cardiopathy having excellent coronary vasodilator and heart rate reducing action. PREPARATION:A carboxylic acid expressed by formula III or reactive derivative thereof is reacted with an amino compound expressed by formula IV in the presence of a base (e.g. pyridine) in water or an organic solvent (e.g. methanol) at -20 deg.C or while being heated and refluxed to afford the compound expressed by formula I.
144 JP27705485 1985-12-11 JPH0312064B2 1991-02-19 HOSE ESUTEBE SORERU
145 JP17582581 1981-11-04 JPH0257540B2 1990-12-05 RIHYARUTO BERUTORUTO; UIRIAMU JON RUISU
146 JP29339185 1985-12-27 JPS641471B2 1989-01-11 URUFU MERUKERU; DEIITERU BORUMAN; DEIITERU MANIA; ROOMAN MUSHAUETSUKU
147 NOVEL ACRYLIC ACID AMIDES JP24113086 1986-10-09 JPS62103051A 1987-05-13 YURUGEN KURUTSUE; HERUMUUTO PIIPAA; YOOZEFU NITSUKURU; RAINTSU MANFURETSUDO BETSUHIYA; GITO ARUBERUTO; KURISUTO DORANDAREFUSUKII; JIKUMUNTO RUSUTO; RUUDOBITSUHI SHIYUREEDAA
148 JP5062775 1975-04-25 JPS624385B2 1987-01-30 DEIITERU BORUMAN; URUFU MERUKERU; ROOMAN MUSHAUETSUKU; DEIITERU MANIA
1504505 Sulphonamides HOECHST AG 25 April 1975 [25 April 1974 27 Dec 1974] 17337/75 Heading C2C The invention comprises novel compounds (I) (including salts thereof) in which R1 and R2, which may be identical or different, each represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, and, if R1 represents a hydrogen atom, R2 may also represent an alkoxymethyl group having from 1 to 4 carbon atoms in the alkoxy radical, a phenoxymethyl group or a phenylthiomethyl group, R3 represents a hydrogen atom, a straight or branched chain alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, having 5 or 6 ring members, one of which may be replaced by an oxygen or sulphur atom, a phenyl or benzyl group which may be substituted in the phenyl nucleus by one or more substituents selected from nitro groups, alkyl groups having from 1 to 3 carbon atoms, alkoxy groups having from 1 to 5 carbon atoms and halogen atoms, or represents a benzhydryl group or an alkanoyloxymethyl group having 2 to 4 carbon atoms in the alkanoyl part, X represents a halogen atom, a CF 3 or CCl 3 group, a straight or branched chain, saturated or unsaturated alkyl group having from 1 to 6 carbon atoms, a benzyl group which may be substituted in the phenyl nucleus by one or more substituents selected from halogen atoms, hydroxy and amino groups, and alkyl and alkoxy groups, or represents one of the groups -O-R4, -S-R4, SO-R4, SO 2 -R4 and NR4R5, in which R4 represents a phenyl group which may be substituted by one or more substituents selected from halogen atoms, CF 3 , OH and amino groups, alkyl and alkoxy groups having from 1 to 4 carbon atoms, and SO 2 NH 2 groups, or represents a straight or branched chain alkyl group having from 1 to 4 carbon atoms which may be substituted by a phenyl, pyridyl, furyl or thienyl group, and R5 represents a hydrogen atom, a straight or branched chain alkyl group having from 1 to 4 carbon atoms, and the group NR4R5 may represent a saturated, heterocyclic, 5- or 6-membered ring which may be interrupted by an O-, N- or S- atom, A represents a single bond, or an alkylene chain of 1 to 3 carbon atoms which may be unsaturated, interrupted by O-, N- or S-atoms or substituted by halogen atoms and/or substituted by alkyl, aralkyl, aryl groups or by mono-nuclear hetero-aromatic rings, or A represents an ortho-phenylene radical or the grouping in which Y represents a single bond or an alkylene group having from 1 to 4 carbon atoms, and R6 and R7, which may be identical or different, each represents a hydrogen or halogen atom or an alkyl group having from 1 to 4 carbon atoms. They are made by standard methods. Pharmaceutical preparations having diuretic and saluretic action contain (I) as active ingredient. Administration is enterally or parenterally.
149 1-SUBSTITUTED-6-FLUORO-7-(PYRROL-1-YL)-1,4-DIHYDRO-4- OXOQUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND MANUFACTURE JP27705485 1985-12-11 JPS61197577A 1986-09-01 HOSE ESUTEBE SORERU
150 Novel esters derived from 2,2-dimethylcyclopropane carboxylic acid and biarylalcohol, manufacture use for parasiticide and composition JP21965083 1983-11-24 JPS59112942A 1984-06-29 JIYAN TESHIE; JIYAN PIEERU DOMUUTO
151 NOVEL TETRAHYDROO1*33OXAZINE AND HERBICIDE CONTAINING IT JP9433779 1979-07-26 JPS5520768A 1980-02-14 KAARU AITSUKEN; UORUFUGANGU ROORU; HANSU YOAHIMU PANDERU; BURUUNO UYURUTSUERU
152 JP4674774 1974-04-26 JPS5013533A 1975-02-13
153 疾患の治療のためのKDM1A阻害剤 JP2020112904 2020-06-30 JP2020172503A 2020-10-22 リーンホフ ヒュー, ヤング, ジュニア; マッコール ジョン エム.; クレア マイケル; セラトカ カサンドラ; タッパー エイミー, イー.
【課題】癌、骨髄性疾患、炎症性疾患等のKDM1A媒介性疾患を予防又は治療するための方法の提供。
【解決手段】下記化合物にて例示される化合物を含む医薬組成物を、好ましくは経口投与にてKDM1A媒介性疾患に適用する。

【選択図】なし
154 選択的アンドロゲン受容体分解剤(SARD)リガンドおよびその使用方法 JP2018564840 2017-06-12 JP2019522644A 2019-08-15 ナラヤナン,ラメシュ; ミラー,デュアン; ポンヌサミ,タマライ; ホワン,ドン−ジン; ヒー,ヤーリー
本発明は、複素環式アニリド環およびそれらの合成前駆体、R−異性体、ならびに非ヒドロキシル化および/または非キラルプロパンアミドを含むピロール、ピラゾール、イミダゾール、トリアゾール、およびモルホリンベースの選択的アンドロゲン受容体分解剤(SARD)化合物、および前立腺癌、進行前立腺癌、去勢抵抗性前立腺癌、トリプルネガティブ乳癌、アンドロゲン受容体を発現する他の癌、アンドロゲン脱毛症または他の高アンドロゲン性皮膚疾患、ケネディ病、筋萎縮性側索硬化症(ALS)、腹部大動脈瘤(AAA)、および子宮筋腫の治療における医薬組成物およびその使用、ならびに対象におけるARの病原性または抵抗性突然変異、AR−スプライスバリアント(AR−SV)、および病原性ポリグルタミン(ポリQ)多型を含むアンドロゲン受容体全長(AR−FL)のレベルを低下させる方法に関する。
【選択図】図1C
155 腎臓及び/又は肝臓疾患を治療するための組成物 JP2017548937 2016-03-18 JP2018509434A 2018-04-05 ダガン,カレン アネット
本発明は、腎臓及び/又は肝臓疾患の予防的及び/又は治療的処置における新規化合物及びその使用に関する。【選択図】なし
156 新規なエストロゲン受容体リガンド JP2014523331 2012-08-02 JP6223336B2 2017-11-01 チェン アイピン; ガルグ ニーラジ; クリューガー ラルス; ロフステット ヨアキム; コッホ エバ; ケーラー コンラッド; ハグバーグ ラルス; ノーテバーグ ダニエル
157 シクロプロパンアミン化合物 JP2013528057 2012-08-08 JP6111195B2 2017-04-05 冨田 直輝; 梶井 重男; キャリー、 ダグラス ロバート; 冨田 大介; 今村 真一; 槌田 謙; 松田 賢; 原 隆二郎
158 光学活性カルボン酸エステルの製造方法 JP2015560069 2015-02-02 JPWO2015115650A1 2017-03-23 椎名 勇; 勇 椎名
動的速度論的光学分割を用いて、α−窒素置換基を有する光学活性カルボン酸エステルを高収率かつ高エナンチオ選択率で製造する方法を提供する。本発明に係る光学活性カルボン酸エステルの製造方法は、下記式(a)で表されるラセミのカルボン酸と、特定のアルコール又はフェノール誘導体とを、酸無物及び不斉触媒の存在下、双極子モーメント3.5以上の極性溶媒中で反応させ、上記ラセミのカルボン酸のうち一方のエナンチオマーを選択的にエステル化するとともに、他方のエナンチオマーをラセミ化する工程を含む。式(a)中、Ra1は環を構成する窒素原子を介して不斉炭素に結合した含窒素複素芳香環基を示し、Ra2は有機基を示す。
159 For use in the treatment of metabolic disorders, compounds, pharmaceutical compositions and methods JP2007500959 2005-02-24 JP5299810B2 2013-09-25 アケルマン,ミツシエル; ハウズ,ジヨナサン; リン,ダニエル・シー・エイチ; リウ,ジウエン; ルオ,チエン; メデイナ,ジユリオ・シー; チウ,ウエイ; レーガン,ジエフリー・デイ; シユミツト,マイケル・ジエイ; ワン,インツアイ; シヤルマ,ラジブ; シヤツトルワース,ステフアン・ジエイ; スン,イン; チヤン,チエン; チユー,リウシヨン; マ,チーホワ; リウ,チンチアン
The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L1-P-L2-M-X-L3-A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.
160 Pharmaceutical made of biaryl amide derivative or its pharmacologically acceptable salt JP2013006116 2013-01-17 JP2013166750A 2013-08-29 KATAYAMA SEIJI; HORI SEIJI; HASEGAWA FUTOSHI; SUZUKI KUNIKO
PROBLEM TO BE SOLVED: To provide a pharmaceutical made of a novel biaryl amide derivative having affinity to an aldosterone receptor or its pharmacologically acceptable salt.SOLUTION: A pharmaceutical is made of a compound represented by formula (1) or its pharmacologically acceptable salt; in the formula, A denotes any group represented by formula (a) or the like; L denotes -CONH- or the like; Rdenotes an aminosulfonyl group or the like which may be substituted; Rdenotes a hydrogen atom or the like; Rdenotes a hydrogen atom or the like; Rdenotes a hydrogen atom, a halogen atom or the like; R, Rand Rdenote a hydrogen atom or the like, respectively independently.